Albendazole (Page 2 of 3)

6.2 Postmarketing Experience

The following adverse reactions have been identified during post-approval use of Albendazole Tablets. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
Blood and Lymphatic System Disorders: Aplastic anemia, bone marrow suppression, neutropenia.
Eye Disorders: Vision blurred.
Gastrointestinal Disorders: Diarrhea.
General System Disorders: Asthenia.
Hepatobiliary Disorders: Elevations of hepatic enzymes, hepatitis, acute liver failure.
Musculoskeletal and Connective Tissue Disorders: Rhabdomyolysis.
Nervous System Disorders: Somnolence, convulsion.
Renal and Urinary Disorders: Acute renal failure.
Skin and Subcutaneous Tissue Disorders: Erythema multiforme, Stevens-Johnson syndrome

7 DRUG INTERACTIONS

7.1 Dexamethasone

Steady-state trough concentrations of albendazole sulfoxide were about 56% higher when 8 mg dexamethasone was coadministered with each dose of albendazole (15 mg/kg/day) in 8 neurocysticercosis patients.

7.2 Praziquantel

In the fed state, praziquantel (40 mg/kg) increased mean maximum plasma concentration and area under the curve of albendazole sulfoxide by about 50% in healthy subjects (n = 10) compared with a separate group of subjects (n = 6) given albendazole alone. Mean Tmax and mean plasma elimination half-life of albendazole sulfoxide were unchanged. The pharmacokinetics of praziquantel were unchanged following coadministration with albendazole (400 mg).

7.3 Cimetidine

Albendazole sulfoxide concentrations in bile and cystic fluid were increased (about 2-fold) in hydatid cyst patients treated with cimetidine (10 mg/kg/day) (n = 7) compared with albendazole (20 mg/kg/day) alone (n = 12). Albendazole sulfoxide plasma concentrations were unchanged 4 hours after dosing.

7.4 Theophylline

Following a single dose of albendazole (400 mg), the pharmacokinetics of theophylline (aminophylline 5.8 mg/kg infused over 20 minutes) were unchanged. Albendazole induces cytochrome P450 1A in human hepatoma cells; therefore, it is recommended that plasma concentrations of theophylline be monitored during and after treatment.

8 USE IN SPECIFIC POPULATIONS

8.1 Pregnancy

Risk Summary
Based on findings from animal reproduction studies, Albendazole Tablets may cause fetal harm when administered to a pregnant woman. However, available human data from a small number of published case series and reports on the use of multiple-dose albendazole in the 1st trimester of pregnancy, and several published studies on single-dose albendazole use later in pregnancy, have not identified any drug-associated risks for major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproductive studies, oral administration of albendazole during the period of organogenesis caused embryotoxicity and skeletal malformations in pregnant rats (at doses of 0.10 times and 0.32 times the maximum recommended human dose based on body surface area in mg/m2) and pregnant rabbits (at doses of 0.60 times the maximum recommended human dose based on body surface area in mg/m2). Albendazole was also associated with maternal toxicity in rabbits (at doses of 0.60 times the recommended human dose based on body surface area in mg/m2) (see Data). Advise a pregnant woman of the potential risk to the fetus.

The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. All pregnancies have a background risk of birth defects, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.

Data
Animal Data
Albendazole has been shown to be teratogenic (to cause embryotoxicity and skeletal malformations) in pregnant rats and rabbits. The teratogenic response in the rat was shown at oral doses of 10 and 30 mg/kg/day (0.10 times and 0.32 times the maximum recommended human dose based on body surface area in mg/m2 , respectively) during organogenesis (gestation days 6 to 15) and in pregnant rabbits at oral doses of 30 mg/kg/day (0.60 times the maximum recommended human dose based on body surface area in mg/m2) administered during organogenesis (gestation days 7 to 19). In the rabbit study, maternal toxicity (33% mortality) was noted at 30 mg/kg/day. In mice, no teratogenic effects were observed at oral doses up to
30 mg/kg/day (0.16 times the recommended human dose based on body surface area in mg/m2), administered during gestation days 6 to 15.

8.2 Lactation

Risk Summary
Concentrations of albendazole and the active metabolite, albendazole sulfoxide, have been reported to be low in human breast milk. There are no reports of adverse effects on the breastfed infant and no information on the effects on milk production. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for Albendazole Tablets and any potential adverse effects on the breastfed infant from Albendazole Tablets or from the underlying maternal condition.

8.3 Females and Males of Reproductive Potential

Pregnancy Testing
Pregnancy testing is recommended for females of reproductive potential prior to initiating Albendazole Tablets.
Contraception
Females Albendazole Tablets may cause fetal harm when administered to a pregnant woman [see Use in Specific Populations (8.1) ]. Advise females of reproductive potential to use effective contraception during treatment with Albendazole Tablets and for 3 days after the final dose.

8.4 Pediatric Use

Hydatid disease is uncommon in infants and young children. In neurocysticercosis, the efficacy of Albendazole Tablets in children appears to be similar to that in adults.

8.5 Geriatric Use

In patients aged 65 and older with either hydatid disease or neurocysticercosis, there was insufficient data to determine whether the safety and effectiveness of Albendazole Tablets is different from that of younger patients.

8.6 Patients with Impaired Renal Function

The pharmacokinetics of Albendazole Tablets in patients with impaired renal function has not been studied.

8.7 Patients with Extra-Hepatic Obstruction

In patients with evidence of extra-hepatic obstruction (n = 5), the systemic availability of albendazole sulfoxide was increased, as indicated by a 2-fold increase in maximum serum concentration and a 7-fold increase in area under the curve. The rate of absorption/conversion and elimination of albendazole sulfoxide appeared to be prolonged with mean Tmax and serum elimination half-life values of 10 hours and 31.7 hours, respectively. Plasma concentrations of parent albendazole were measurable in only 1 of 5 patients.

10 OVERDOSAGE

In case of overdosage, symptomatic therapy and general supportive measures are recommended.

11 DESCRIPTION

Albendazole is an orally administered anthelmintic drug. Chemically, it is methyl 5-(propylthio)-2-benzimidazolecarbamate. Its molecular formula is C12 H15 N3 O2 S. Its molecular weight is 265.34. It has the following chemical structure:

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(click image for full-size original)

Albendazole is a white to yellowish powder. It is freely soluble in anhydrous formic acid and very slightly soluble in ether and in methylene chloride. Albendazole is practically insoluble in alcohol and in water. Albendazole Tablets USP are white to off-white, round, convex, film-coated tablets, debossed with “110” with an arch overhead on one side and plain on the other side and contain 200 mg of albendazole.

The inactive ingredients of Albendazole Tablets USP consist of: hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, povidone, sodium lauryl sulfate, sodium starch glycolate and corn starch.

12 CLINICAL PHARMACOLOGY

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